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    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS
    2.
    发明公开
    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 有权
    PYRROLIDINARYLETHER AS NK-3受体拮抗剂

    公开(公告)号：EP2190815A1

    公开(公告)日：2010-06-02

    申请号：EP08787130.7

    申请日：2008-08-12

    申请人： F. Hoffmann-La Roche AG

    发明人： JABLONSKI, Philippe ,  KAWASAKI, Kenichi ,  KNUST, Henner ,  LIMBERG, Anja ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  WU, Xihan

    IPC分类号： C07D207/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D487/04 ,  C07D491/04 ,  C07D491/10 ,  A61K31/4468 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61P23/00 ,  A61P25/00 ,  A61P25/16

    CPC分类号： C07D401/14 ,  C07D207/08 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D487/04 ,  C07D491/04 ,  C07D491/10

    摘要： The invention relates to a compound of general formula (I) wherein is aryl or a five or six membered heteroaryl; is a six to nine membered mono or bi-heterocyclic group, wherein X may be a carbon atom, SO2 or a further hetero atom, selected from the group consisting of N or O; if X is a carbon atom, O, SO2 or unsubstituted N, then R1 is hydrogen, hydroxy, cyano, -(CH 2 ) q -OH, -(CH 2 ) q -NRR', -(CH 2 )q-CN, lower alkyl, -S(O) 2 -lower alkyl, -NR-S(O) 2 -lower alkyl, -C(O)-lower alkyl, -NR-C(O)-lower alkyl, phenyl, or is a heterocyclic group selected from piperidinyl-2-one; if X is a N-atom, substituted by R 1, then R 1 is hydrogen, -(CH 2 ) q -OH, -(CH 2 ) q -NRR', -(CH 2 )q-CN, lower alkyl, -S(O) 2 - lower alkyl, aryl or a five or six membered heteroaryl or -C(O)-lower alkyl, provided that q is 2 or 3. R/R' are independently from each other hydrogen or lower alkyl; R 2 is hydrogen, halogen, lower alkyl, cyano, lower alkoxy substituted by halogen, lower alkyl substituted by halogen or is a five or six membered heteroaryl; R 3 is hydrogen or halogen; R 4 is hydrogen or lower alkyl; n is 1 or 2; in case n is 2, R 1 may be the same or different; o is 1 or 2; in case o is 2, R 2 may be the same or different; p is 1 or 2; in case p is 2, R 3 may be the same or different; q is 1, 2 or 3; s is 0, 1, 2, 3 or 4; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS
    4.
    发明授权
    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 有权
    作为NK3受体拮抗剂的吡咯烷基芳基醚

    公开(公告)号：EP2190815B1

    公开(公告)日：2011-08-10

    申请号：EP08787130.7

    申请日：2008-08-12

    申请人： F. Hoffmann-La Roche AG

    发明人： JABLONSKI, Philippe ,  KAWASAKI, Kenichi ,  KNUST, Henner ,  LIMBERG, Anja ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  WU, Xihan

    IPC分类号： C07D207/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D487/04 ,  C07D491/04 ,  C07D491/10 ,  A61K31/4468 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61P23/00 ,  A61P25/00 ,  A61P25/16

    CPC分类号： C07D401/14 ,  C07D207/08 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D487/04 ,  C07D491/04 ,  C07D491/10

    摘要： The invention relates to a compound of general formula (I) wherein is aryl or a five or six membered heteroaryl; is a six to nine membered mono or bi-heterocyclic group, wherein X may be a carbon atom, SO2 or a further hetero atom, selected from the group consisting of N or O; if X is a carbon atom, O, SO2 or unsubstituted N, then R1 is hydrogen, hydroxy, cyano, -(CH 2 ) q -OH, -(CH 2 ) q -NRR', -(CH 2 )q-CN, lower alkyl, -S(O) 2 -lower alkyl, -NR-S(O) 2 -lower alkyl, -C(O)-lower alkyl, -NR-C(O)-lower alkyl, phenyl, or is a heterocyclic group selected from piperidinyl-2-one; if X is a N-atom, substituted by R 1, then R 1 is hydrogen, -(CH 2 ) q -OH, -(CH 2 ) q -NRR', -(CH 2 )q-CN, lower alkyl, -S(O) 2 - lower alkyl, aryl or a five or six membered heteroaryl or -C(O)-lower alkyl, provided that q is 2 or 3. R/R' are independently from each other hydrogen or lower alkyl; R 2 is hydrogen, halogen, lower alkyl, cyano, lower alkoxy substituted by halogen, lower alkyl substituted by halogen or is a five or six membered heteroaryl; R 3 is hydrogen or halogen; R 4 is hydrogen or lower alkyl; n is 1 or 2; in case n is 2, R 1 may be the same or different; o is 1 or 2; in case o is 2, R 2 may be the same or different; p is 1 or 2; in case p is 2, R 3 may be the same or different; q is 1, 2 or 3; s is 0, 1, 2, 3 or 4; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

    摘要翻译： 本发明涉及通式（I）的化合物，其中芳基或五元或六元杂芳基; 是六至九元的单或双杂环基团，其中X可以是碳原子，SO 2或另一个选自N或O的杂原子; 如果X是碳原子，O，SO 2或未取代的N，则R 1是氢，羟基，氰基， - （CH 2）q -OH， - （CH 2）q -NRR'， - （CH 2）q -CN ，-S（O）2 - 低级烷基，-NR-S（O）2 - 低级烷基，-C（O） - 低级烷基，-NR-C（O） - 低级烷基，苯基或 选自哌啶基-2-酮的杂环基; 如果X是被R 1取代的N-原子，则R 1是氢， - （CH 2）q -OH， - （CH 2）q -NRR'， - （CH 2）q -CN，低级烷基， -S（O）2 - 低级烷基，芳基或五元或六元杂芳基或-C（O） - 低级烷基，条件是q为2或3。 R 2是氢，卤素，低级烷基，氰基，被卤素取代的低级烷氧基，被卤素取代的低级烷基或为五元或六元杂芳基; R 3是氢或卤素; R 4是氢或低级烷基; n是1或2; 在n为2的情况下，R 1可以相同或不同; o是1或2; 在o为2的情况下，R 2可以相同或不同; p是1或2; 在p为2的情况下，R 3可以相同或不同; q是1,2或3; s是0,1,2,3或4; 或其药学活性盐，包括式（I）化合物的所有立体异构形式，单独的非对映异构体和对映异构体以及其外消旋和非外消旋混合物。 已经发现本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意力缺陷多动症（ADHD）的高潜力NK-3受体拮抗剂。

    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS
    6.
    发明授权
    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 有权
    PYRROLIDINARYLETHER AS NK-3受体拮抗剂

    公开(公告)号：EP2185540B1

    公开(公告)日：2011-07-20

    申请号：EP08786547.3

    申请日：2008-07-29

    申请人： F. Hoffmann-La Roche AG

    发明人： JABLONSKI, Philippe ,  KAWASAKI, Kenichi ,  KNUST, Henner ,  LIMBERG, Anja ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  WU, Xihan

    IPC分类号： C07D401/08 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D401/08

    摘要： The invention relates to a compound of general formula (I) wherein Ar1 is aryl or a five or six membered heteroaryl; Ar2 is aryl or a five or six membered heteroaryl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkyl amino, -(CH2)qR, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R3 is hydrogen or lower alkyl or CH2OH; R4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS
    8.
    发明公开
    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 有权
    作为NK3受体拮抗剂的吡咯烷基芳基醚

    公开(公告)号：EP2185540A1

    公开(公告)日：2010-05-19

    申请号：EP08786547.3

    申请日：2008-07-29

    申请人： F. Hoffmann-La Roche AG

    发明人： JABLONSKI, Philippe ,  KAWASAKI, Kenichi ,  KNUST, Henner ,  LIMBERG, Anja ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  WU, Xihan

    IPC分类号： C07D401/08 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D401/08

    摘要： The invention relates to a compound of general formula (I) wherein Ar1 is aryl or a five or six membered heteroaryl; Ar2 is aryl or a five or six membered heteroaryl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkyl amino, -(CH2)qR, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R3 is hydrogen or lower alkyl or CH2OH; R4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

    摘要翻译： 本发明涉及通式（I）的化合物，其中Ar 1是芳基或五元或六元杂芳基; Ar 2是芳基或五元或六元杂芳基; R1是氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，S-低级烷基，-S（O）2 - 低级烷基，-S（O）2 - 二低级烷基 氨基， - （CH 2）q R，氰基，氨基，单或二低级烷基氨基，NHC（O） - 低级烷基，环烷基或任选被低级烷基取代的五元杂芳基; 其中R是氰基，二低级烷基氨基或吡咯烷-1-基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基或CH2OH; R4是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; n是1,2或3; 在n为2或3的情况下，R1可以相同或不同; o是1,2或3; 在o为2或3的情况下，R2可以相同或不同; p是1,2或3; 在p为2或3的情况下，R 4可以相同或不同; q是1或2; 或其药学活性盐，包括式（I）化合物的所有立体异构形式，单独的非对映异构体和对映异构体以及其外消旋和非外消旋混合物。 已经发现本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意力缺陷多动症（ADHD）的高潜力NK-3受体拮抗剂。